PKS13 Inhibitors - TAM16

Whole-cell based high-throughput screen with aerobically grown Mtb H37Rv. IC50 = 0.19 mM, MIC = 0.09 mM, In vivo active in mouse models.  From Abstract:  "In multiple mouse models of TB infection, TAM16 showed in vivo efficacy equal to the first-line TB drug isoniazid, both as a monotherapy and in combination therapy with rifampicin. TAM16 has excellent pharmacological and safety profiles, and the frequency of resistance for TAM16 is 100-fold lower than INH, suggesting that it can be developed as a new antitubercular aimed at the acute infection."

TBA-7371

AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2’-epimerase (DprE1) with an IC50 value of 10 nM.1 It also inhibits PDE6 with an IC50 value of 4 µM.1 AZ 7371 has been shown to be active against M. tuberculosis with an MIC range of 0.78-3.12 µM and demonstrates efficacy in a rodent model of tuberculosis.

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